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Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2

✍ Scribed by Rut Lucas; Amalia Úbeda; Miguel Payá; Mario Alves; Esther del Olmo; José L. López; Arturo San Feliciano


Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
134 KB
Volume
10
Category
Article
ISSN
0960-894X

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✦ Synopsis


We have synthesised some lipidic diamines and aminoalcohols and examined their behaviour as inhibitors of secretory and cytosolic PLA2. Some structure-activity relationships considerations have been deduced. Compound 14 was a potent and selective inhibitor of cPLA2 and compound 4 showed a dual inhibitory profile against both types of PLA2 while no cytotoxicity at 10 microM on human neutrophils or on murine macrophage line was observed for both.


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